半岛bd体育手机客户端 说明
包装
5, 25 mg in glass bottle
生化/生理作用
SI-2 targets the receptor-interacting domain (RID) of steroid receptor coactivators (SRCs) and suppresses cellular transcriptional activity (Effec. conc. >/= 5 nM in cell-based SRC-1, SRC-2, and SRC-3 reporter assays) by downregulating SRCs protein, but not transcript level (Effec. conc. >/= 12.5 nM against SRC-3, >/= 25 nM against SRC-1 and SCR-2 in MDA-MB-468 culture). SI-2 is cytotoxic to breast cancer cultures (IC50= 1.5 nM/BT-474, 3.4 nM/MDA-MB-468, 22 nM/MCF-7), but not to normal hepatocytes even at 500 nM concentration. SI-2 is reported to be orally available in mice and, when administered intraperitoneally (2 mg/kg b.i.d.), effectively suppress MDA-MB-468-derived tumor expansion in mice in vivowith good pharmacokinetics (Cmax= 30 μM, tmax= 0.25 h, t1/2= 1.0 h; 20 mg/kg i.p.) and no apparent adverse effects to the animals.
基本信息
经验(实验)分子式 | C15H15N5 |
分子量 | 265.31 |
半岛bd体育手机客户端 性质
质量水平 | 100 |
测定 | ≥98% (HPLC) |
形式 | powder |
颜色 | , light yellow to dark orange |
溶解性 | DMSO: 20 mg/mL, clear |
储存温度 | 2-8℃ |
SMILES string | C/C(C1=CC=CC=N1)=N\NC2=NC3=C(C=CC=C3)N2C |
安全信息
象形图 | |
警示用语: | Warning |
危险声明 | H315 - H319 |
预防措施声明 | P305 + P351 + P338 |
危险分类 | Eye Irrit. 2 - Skin Irrit. 2 |
储存分类代码 | 13 - Non Combustible Solids |
WGK | WGK 3 |
闪点(F) | Not applicable |
闪点(C) | Not applicable |
Sigma-Aldrich